Imidazo[1,2-a]pyrimidines as Functionally Selective and Orally Bioavailable GABAAα2/α3 Binding Site Agonists for the Treatment of Anxiety Disorders

Simon Goodacre; Leslie J. Street; David J. Hallett; James Crawforth; Sarah Kelly; Andrew P. Owens; Wesley Blackaby; Richard T. Lewis; Joanna L. Stanley; Alison J. Smith; Pushpinder Ferris; Bindi Sohal; Susan M. Cook; Andrew Pike; N. Brown; Keith A. Wafford; George Marshall; José L. Castro; John Atack

doi:10.1021/jm051065l

Abstract

This is the authors' abstract. We don't add key points for this paper.

A series of high-affinity GABA(A) agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA(A)alpha2 and -alpha3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned animal models of anxiety with minimal sedation observed at full BZ binding site occupancy.

Ask about this paper

Answers are grounded in this paper and cite their sources.

Discussion

No takes yet. Share an insight, caveat, or question.

Cite This Study

Goodacre et al. (2005) studied this question.

synapsesocial.com/papers/6a0b109b679a27e0902e0a07 https://doi.org/10.1021/jm051065l

View Full Paper

Ask AI

Bookmark

Share

Imidazo[1,2-a]pyrimidines as Functionally Selective and Orally Bioavailable GABAAα2/α3 Binding Site Agonists for the Treatment of Anxiety Disorders

Abstract

Ask about this paper

Discussion

Cite This Study

Imidazo[1,2-a]pyrimidines as Functionally Selective and Orally Bioavailable GABAAα2/α3 Binding Site Agonists for the Treatment of Anxiety Disorders

Abstract

Ask about this paper

Discussion

Cite This Study

Keep reading

Keep reading